Dosing & Uses
Dosage Forms & Strengths
tablet
- 25mg
- 50mg
Hypertension (HTN)
Initial 50 mg PO qDay; may increase to 50 mg PO q12hr; may take up to four weeks for full therapeutic response; hyperkelemia may occur with doses >100 mg/day
Heart Failure Post MI
Initial 25 mg PO qDay; may titrate to maximum of 50 mg once daily within 4 weeks as tolerated
Dose adjustments may be required based on potassium levels
Renal Impairment
Contraindicated if CrCl <50 mL/min or serum creatinine >2 mg/dL in males or >1.8 mg/dL in females
Hepatic Impairment
Dose adjustment not necessary
Dosing considerations
In post-MI CHF patients taking a moderate CYP3A inhibitor, do not exceed 25 mg once daily; in patients with hypertension taking a moderate CYP3A inhibitor, initiate at 25 mg once daily; for inadequate blood pressure response, dosing may be increased to a maximum of 25 mg twice daily
Other Indications and Uses
Improving survival of stable patients with LV systolic dysfunction (LVEF ≤40%) and CHF after an acute myocardial infarction (MI)
Safety and efficacy not established
Hypertension
Initial 50 mg PO qDay; may increase to 50 mg PO q12hr; may take up to four weeks for full therapeutic response; hyperkelemia may occur with doses >100 mg/day
Heart Failure Post MI
Initial 25 mg PO qDay; may titrate to maximum of 50 mg once daily within 4 weeks as tolerated
Dose adjustments may be required based on potassium levels
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
1-10%
Hyperkalemia (2-10%)
Increased risk of hyperkalemia with presence of renal dysfunction
1-3%
- Dizziness
- Fatigue/malaise
- Abdominal pain
- Diarrhea
- Albuminuria
- Hypercholesterolemia
- Hypertriglyceridemia
- Cough
<1%
Abnormal vaginal bleeding
Gynecomastia
Mastodynia
Warnings
Contraindications
Hypersensitivity
For all patients: Serum potassium >5.5 mEq/L at initiation Creatinine clearance ≤30 mL/min Concomitant use with strong CYP3A inhibitors For the treatment of hypertension: Type 2 diabetes with microalbuminuria Serum creatinine >2.0 mg/dL in males, >1.8 mg/dL in females Creatinine clearance <50 mL/min Concomitant use of potassium supplements or potassium-sparing diuretics
For all patients
- Serum potassium >5.5 mEq/L at initiation
- Creatinine clearance ≤30 mL/min
- Concomitant use with strong CYP3A inhibitors
For the treatment of hypertension
- Type 2 diabetes with microalbuminuria
- Serum creatinine >2.0 mg/dL in males, >1.8 mg/dL in females
- Creatinine clearance <50 mL/min
- Concomitant use of potassium supplements or potassium-sparing diuretics
Cautions
Hyperkalemia, liver dysfunction, metabolic or respiratory acidosis, renal impairment, hypersensitivity to spironolactone
The risk of hyperkalemia is higher in patients with impaired renal function, proteinuria , diabetes and those concomitantly treated with ACEs, ARBs, NSAIDs and moderate CYP3A inhibitors
Patients taking moderate CYP3A inhibitors that cannot be avoided should have their dose of eplerenone reduced
Pregnancy & Lactation
Pregnancy
Available data from published case reports on eplerenone use during pregnancy are insufficient to establish a drug-associated risk of major birth defects, miscarriage, adverse maternal or fetal outcomes; in animal studies, no adverse developmental effects were observed when eplerenone was administered to pregnant rats and rabbits during organogenesis at exposures 32 and 31 times, respectively the human exposure at the 100 mg/day therapeutic dose
Hypertension in pregnancy increases maternal risk for pre-eclampsia, gestational diabetes, premature delivery, and delivery complications (e.g., need for cesarean section, and post-partum hemorrhage); hypertension increases fetal risk for intrauterine growth restriction and intrauterine death; pregnant women with hypertension should be carefully monitored and managed accordingly
Infertility
- Based on animal data, therapy may compromise male fertility; in mature rates, male fertility was decreased with eplerenone exposure at 17 times the 100 mg/day human therapeutic dose; reversibility of effect, not evaluated
Lactation
There are no human data available on whether eplerenone is present in human milk, or has effects on breastfed infants or on milk production; eplerenone was present in milk of lactating rats; when a drug is present in animal milk, it is likely that the drug will be present in human milk
Pregnancy Categories
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Pharmacology
Mechanism of Action
Selective aldosterone receptor antagonist; blocks aldosterone binding at the mineralocorticoid receptor
Pharmacokinetics
Half-Life: 3.5-6 hr
Peak Plasma Time: 1-2 hr
Bioavailability: 69%
Protein Bound: 50%
Vd: 43-90 L
Metabolism: primarily hepatic CYP3A4
Metabolite: no active mets identified
Total Body Clearance: 10 L/hr
Excretion: feces (32%) and urine (67%)
Images
Patient Handout
Formulary
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